Pioglitazone-loaded nanostructured lipid carriers: In-vitro and in-vivo evaluation for improved bioavailability

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F23%3A10479101" target="_blank" >RIV/00216208:11160/23:10479101 - isvavai.cz</a>

Výsledek na webu

<a href="https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=a5FLdg89lL" target="_blank" >https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=a5FLdg89lL</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.jddst.2022.104041" target="_blank" >10.1016/j.jddst.2022.104041</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Pioglitazone-loaded nanostructured lipid carriers: In-vitro and in-vivo evaluation for improved bioavailability

Popis výsledku v původním jazyce

Pioglitazone (PZ), a highly lipophilic Class II drug with poor aqueous solubility possesses low oral bioavailability. The oral bioavailability of pioglitazone can be improved by incorporating into nanostructured lipid carriers (NLCs). Pioglitazone-loaded nanostructured lipid carriers (PZ-loaded NLCs) were developed by using the solvent emulsification evaporation method. The lipid phase of the formulation consists of a solid and liquid lipid mixture (fatty acids and oils) and surfactants (Tween 20, Span 40) were used for the stability of the formulation. PZ-loaded NLCs were characterized for physicochemical characteristics including particle size, zeta potential, polydispersity index (PDI), fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD) and scanning electron microscopy (SEM) and stability studies. Moreover, drug entrapment efficiency, drug loading capacity, drug release, toxicity studies, permeation studies, and in-vivo studies were performed to evaluate enhanced bioavailability. PZ-loaded NLCs have shown an average particle size of 152 nm, PDI of 0.19, and a negative value of zeta potential. Drug entrapment efficiency and loading capacity were about 83% and 5.8%, respectively. SEM results delineated the smooth homogenous surface in nano-sized range, whereas FTIR spectra demonstrated no interaction between components of PZ-loaded NLCs formulation. For drug release studies, the dialysis bag method confirmed a biphasic release behavior in beginning followed by slow, controlled release up to 24 h. Furthermore, permeation studies showed enhanced permeability and in-vivo studies confirmed the enhanced bioavailability of pioglitazone. Based on the above finding, it can be concluded that NLCs are a versatile tools for enhancing the bioavailability of poorly soluble Class II drugs.

Název v anglickém jazyce

Pioglitazone-loaded nanostructured lipid carriers: In-vitro and in-vivo evaluation for improved bioavailability

Popis výsledku anglicky

Pioglitazone (PZ), a highly lipophilic Class II drug with poor aqueous solubility possesses low oral bioavailability. The oral bioavailability of pioglitazone can be improved by incorporating into nanostructured lipid carriers (NLCs). Pioglitazone-loaded nanostructured lipid carriers (PZ-loaded NLCs) were developed by using the solvent emulsification evaporation method. The lipid phase of the formulation consists of a solid and liquid lipid mixture (fatty acids and oils) and surfactants (Tween 20, Span 40) were used for the stability of the formulation. PZ-loaded NLCs were characterized for physicochemical characteristics including particle size, zeta potential, polydispersity index (PDI), fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD) and scanning electron microscopy (SEM) and stability studies. Moreover, drug entrapment efficiency, drug loading capacity, drug release, toxicity studies, permeation studies, and in-vivo studies were performed to evaluate enhanced bioavailability. PZ-loaded NLCs have shown an average particle size of 152 nm, PDI of 0.19, and a negative value of zeta potential. Drug entrapment efficiency and loading capacity were about 83% and 5.8%, respectively. SEM results delineated the smooth homogenous surface in nano-sized range, whereas FTIR spectra demonstrated no interaction between components of PZ-loaded NLCs formulation. For drug release studies, the dialysis bag method confirmed a biphasic release behavior in beginning followed by slow, controlled release up to 24 h. Furthermore, permeation studies showed enhanced permeability and in-vivo studies confirmed the enhanced bioavailability of pioglitazone. Based on the above finding, it can be concluded that NLCs are a versatile tools for enhancing the bioavailability of poorly soluble Class II drugs.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

30104 - Pharmacology and pharmacy

Projekt

—

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2023

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Journal of Drug Delivery Science and Technology

ISSN

1773-2247

e-ISSN

2588-8943

Svazek periodika

79

Číslo periodika v rámci svazku

January

Stát vydavatele periodika

FR - Francouzská republika

Počet stran výsledku

8

Strana od-do

104041

Kód UT WoS článku

000897608700005

EID výsledku v databázi Scopus

2-s2.0-85145229925